23456-78-2Relevant articles and documents
PHOTOCHEMOTHERAPEUTIC HETEROCYCLIC AGENTS HAVING ANTIPROLIFERATIVE AND ANTINEOPLASTIC ACTIVITY
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Page/Page column 3, (2012/06/01)
The present invention concerns the synthesis of new analogs of angelicins, pyrrolo [3,2-h]quinoline, for the treatment of pathologies having hyperproliferative character included those having neoplastic nature. The treatment is based on the combined actio
Synthesis of pyrrolo[3,2-h]quinolinones with good photochemotherapeutic activity and no DNA damage
Barraja, Paola,Caracausi, Libero,Diana, Patrizia,Carbone, Anna,Montalbano, Alessandra,Cirrincione, Girolamo,Brun, Paola,Palu, Giorgio,Castagliuolo, Ignazio,Dall'Acqua, Francesco,Vedaldi, Daniela,Salvador, Alessia
scheme or table, p. 4830 - 4843 (2010/08/06)
In the search for new photochemotherapeutic agents, a series of derivatives of the ring system pyrrolo[3,2-h]quinoline - bioisosters of the angular furocoumarin angelicin - were synthesized through a four-step synthetic approach, in reasonable overall yields. Eight of the synthesized derivatives showed a remarkable phototoxicity against a panel of four human tumor cell lines and a great dose UV-A dependence, reaching IC50 values at submicromolar level. The mode of cellular death photoinduced by pyrrolo[3,2-h]quinolines was evaluated through a series of flow cytometric analysis and other tests were performed to clarify their mechanism of action.
Conversion of δ-(sulfonyl)amino-α-epoxy ketones to bicyclic ketopyrroles via intramolecular conjugate-addition to azoene intermediates. Synthesis of the bicyclic ketopyrrole core of the 1-azafulvene roseophilin
Kim, Seong Heon,Fuchs
, p. 2545 - 2548 (2007/10/03)
Reaction of δ-(sulfonyl)amino-α-epoxy ketones with dimethylhydrazine results in cyclization to pyrrolidine-fused β-hydroxy dimethylhydrazones. Hydrolysis, mesylation, and elimination affords dihydropyrroles which can be converted to sulfonyl-protected ketopyrroles via oxidation with NIS; alternatively, treatment with DBU affords N-H bearing ketopyrroles. Copyright